@article{MTMT:33206020,
	title = {Substitutional Diversity-Oriented Synthesis and In Vitro Anticancer Activity of Framework-Integrated Estradiol-Benzisoxazole Chimeras},
	url = {https://m2.mtmt.hu/api/publication/33206020},
	author = {Kovács, Ferenc and Adamecz, Dóra Izabella and Nagy, Ferenc István and Papp, Benedek and Csontné Kiricsi, Mónika and Nagyné Frank, Éva},
	doi = {10.3390/molecules27217456},
	journal-iso = {MOLECULES},
	journal = {MOLECULES},
	volume = {27},
	unique-id = {33206020},
	abstract = {Hybridization of steroids and other pharmacophores often modifies the bioactivity of the parent compounds, improving selectivity and side effect profile. In this study, estradiol and 3′-(un)substituted benzisoxazole moieties were combined into novel molecules by structural integration of their aromatic rings. Simple estrogen starting materials, such as estrone, estradiol and estradiol-3-methylether were used for the multistep transformations. Some of the heterocyclic derivatives were prepared from the estrane precursor by a formylation or Friedel–Crafts acylation—oximation—cyclization sequence, whereas others were obtained by a functional group interconversion strategy. The antiproliferative activities of the synthesized compounds were assessed on various human cervical, breast and prostate cancer cell lines (HeLa, MCF-7, PC3, DU-145) and non-cancerous MRC-5 fibroblast cells. Based on the primary cytotoxicity screens, the most effective cancer-selective compounds were selected, their IC50 values were determined and their apoptosis-inducing potential was evaluated by quantitative real-time PCR. Pharmacological studies revealed a strong structure–function relationship, where derivatives with a hydroxyl group on C-17 exhibited stronger anticancer activity compared to the 17-acetylated counterparts. The present study concludes that novel estradiol-benzisoxazole hybrids exert remarkable cancer cell-specific antiproliferative activity and trigger apoptosis in cancer cells.},
	keywords = {ESTRADIOL; hybrid; Apoptosis induction; benzisoxazole; cancer selectivity},
	year = {2022},
	eissn = {1420-3049},
	orcid-numbers = {Adamecz, Dóra Izabella/0000-0002-1883-9600; Csontné Kiricsi, Mónika/0000-0002-8416-2052; Nagyné Frank, Éva/0000-0002-1332-0551}
}

@article{MTMT:33049036,
	title = {Efficient Access to Domain-Integrated Estradiol-Flavone Hybrids Via the Corresponding Chalcones and Their in Vitro Anticancer Potential},
	url = {https://m2.mtmt.hu/api/publication/33049036},
	author = {Molnár, Barnabás and Gopisetty, Mohana Krishna and Nagy, Ferenc István and Adamecz, Dóra Izabella and Kása, Zsolt and Csontné Kiricsi, Mónika and Nagyné Frank, Éva},
	doi = {10.1016/j.steroids.2022.109099},
	journal-iso = {STEROIDS},
	journal = {STEROIDS},
	volume = {187},
	unique-id = {33049036},
	issn = {0039-128X},
	abstract = {Structural modification of the phenolic A-ring of estrogens at C-2 and/or C-3 significantly reduces or eliminates the hormonal effects of the compounds, thus the incorporation of other pharmacophores into these positions can provide biologically active derivatives suitable for new indications, without possessing unwanted side effects. As part of this work, A-ring integration of estradiol with chalcones and flavones was carried out in the hope of obtaining novel molecular hybrids with anticancer action. The syntheses were performed from 2-acetylestradiol-17 beta-acetate which was first reacted with various (hetero)aromatic aldehydes in a pyrrolidine-catalyzed reaction in DMSO. The chalcones thus obtained were then subjected to oxidative cyclization with I2 in DMSO to afford estradiol-flavone hybrids in good yields. All newly synthesized derivatives were tested in vitro for cytotoxicity on human malignant cell lines of diverse origins as well as on a non-cancerous cell line, and the results demonstrated that estradiol-flavone hybrids containing a structure-integrated flavone moiety were the most active and cancer cell-selective agents. The minimal inhibitory concentration values (IC50) were calculated for selected compounds (3c, 3d and 3e) and their apoptosis inducing capacity was verified by RT-qPCR (real-time quantitative poly-merase chain reaction). The results suggest an important structure-activity relationship regarding estradiol-flavone hybrids that could form a promising synthetic platform and rationale for future drug developments.},
	year = {2022},
	eissn = {1878-5867},
	orcid-numbers = {Gopisetty, Mohana Krishna/0000-0002-4310-3478; Adamecz, Dóra Izabella/0000-0002-1883-9600; Kása, Zsolt/0000-0003-4352-7761; Csontné Kiricsi, Mónika/0000-0002-8416-2052; Nagyné Frank, Éva/0000-0002-1332-0551}
}

@article{MTMT:31965884,
	title = {Synthesis and conversion of primary and secondary 2-aminoestradiols into A-ring-integrated benzoxazolone hybrids and their in vitro anticancer activity},
	url = {https://m2.mtmt.hu/api/publication/31965884},
	author = {Kovács, Ferenc and Gopisetty, Mohana Krishna and Adamecz, Dóra Izabella and Csontné Kiricsi, Mónika and Enyedy, Éva Anna and Nagyné Frank, Éva},
	doi = {10.1039/D1RA01889B},
	journal-iso = {RSC ADV},
	journal = {RSC ADVANCES},
	volume = {11},
	unique-id = {31965884},
	issn = {2046-2069},
	year = {2021},
	eissn = {2046-2069},
	pages = {13885-13896},
	orcid-numbers = {Kovács, Ferenc/0000-0002-1332-0551; Gopisetty, Mohana Krishna/0000-0002-4310-3478; Adamecz, Dóra Izabella/0000-0002-1883-9600; Csontné Kiricsi, Mónika/0000-0002-8416-2052; Enyedy, Éva Anna/0000-0002-8058-8128; Nagyné Frank, Éva/0000-0002-1332-0551}
}

@article{MTMT:31571893,
	title = {Multistep Synthesis and In Vitro Anticancer Evaluation of 2-Pyrazolyl-Estradiol Derivatives, Pyrazolocoumarin-Estradiol Hybrids and Analogous Compounds},
	url = {https://m2.mtmt.hu/api/publication/31571893},
	author = {Molnár, Barnabás and Gopisetty, Mohana Krishna and Adamecz, Dóra Izabella and Csontné Kiricsi, Mónika and Nagyné Frank, Éva},
	doi = {10.3390/molecules25184039},
	journal-iso = {MOLECULES},
	journal = {MOLECULES},
	volume = {25},
	unique-id = {31571893},
	year = {2020},
	eissn = {1420-3049},
	orcid-numbers = {Gopisetty, Mohana Krishna/0000-0002-4310-3478; Adamecz, Dóra Izabella/0000-0002-1883-9600; Csontné Kiricsi, Mónika/0000-0002-8416-2052; Nagyné Frank, Éva/0000-0002-1332-0551}
}

@article{MTMT:3406424,
	title = {Steroidal anticancer agents: an overview of estradiol-related compounds},
	url = {https://m2.mtmt.hu/api/publication/3406424},
	author = {Minorics, Renáta and Zupkó, István},
	doi = {10.2174/1871520617666171114111721},
	journal-iso = {ANTI-CANCER AGENT ME},
	journal = {ANTI-CANCER AGENTS IN MEDICINAL CHEMISTRY},
	volume = {18},
	unique-id = {3406424},
	issn = {1871-5206},
	abstract = {Research of steroidal compounds as anticancer agents started almost 50 years ago. During the past decades several innovative new steroids, like cyproterone, finasteride, estramustin, exemestane and fulvestrant have successfully become part of routine clinical practice. Meanwhile, a vast amount of new information have accumulated about the functions of the endogenous steroid system (including the characterization of enzymes, receptors, transcription pathways, etc.) and about the role of steroids in carcinogenesis. Therefore, it is regularly required to review the latest published results, focusing on a well-defined part within this research field that has definitely developed into a highly diversified speciality by now. Herein, we make an attempt to summarize the most recent results reported about anticancer agents of estrane backbone, focusing on their mechanisms of action and their structure-activity relationships. Due to the vast number and various accessibilities of scientific publications, neither other reviews nor this one can be considered as absolutely exhaustive. In spite of these restrictive factors, the current review makes a good opportunity to define the hottest scientific trends in the field of estradiol-related anticancer agents.},
	year = {2018},
	eissn = {1875-5992},
	pages = {652-666},
	orcid-numbers = {Minorics, Renáta/0000-0001-9685-813X; Zupkó, István/0000-0003-3243-5300}
}